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Increase in AV conduction

decompensation after surgery, or patients with CHF or MI

heart rate

hypertension or cardiac arrhythmias Used only IV

ß2-selective (intermediate-acting)

Albuterol

Bitolterol

Fenoterol

Isoetharine

Metaproterenol

Procaterol

Terbutaline

Ritodrine

Relaxation of bronchial smooth muscle Relaxation of uterine smooth muscle Activation of other ß2 receptors after systemic administration

Bronchodilators for treatment of asthma and COPD Short/intermediate-acting drugs for acute bronchospasm

Skeletal muscle tremor Tachycardia and other cardiac effects seen after systemic administration (much less with inhalational use)

Use with caution in patients with CV disease (reduced by inhalational administration) Minimal side effects

(Long-acting)

a Receptor agonists a.-selective

8 a2-selective

Indirect-acting

Formoterol Salmeterol

Methoxamine

Phenylephrine

Mephentermine

Metaraminol

Midodrine

Clonidine

Apraclonidine

Guanfacine

Guanabenz

Brimonidine a-methyldopa

Amphetamine Methamphetamine Methyphenidate (releases NE peripherally; NE, DA, 5-HT centrally)

Vasoconstriction

Best choice for prophylaxis due to long action

Nasal congestion (used topically) Postural hypotension

Decrease sympathetic outflow from brain to periphery resulting in decreased PVR and blood pressure Decrease nerve-evoked release of sympathetic transmitters Decrease production of aqueous humor CNS stimulation Increase in blood pressure Myocardial stimulation

Adjunctive therapy in shock Hypertension To reduce sympathetic response to withdrawal from narcotics, alcohol, and tobacco Glaucoma

Treatment of ADHD Narcolepsy Obesity (rarely)

Hypertension Reflex bradycardia Dry mouth, sedation, rebound hypertension upon abrupt withdrawal

Restlessness

Tremor

Insomnia

Anxiety

Tachycardia

Hypertension

Cardiac arrhythmias

Long action favored for prophylaxis

Mephentermine and metaraminol also act indirectly to release NE Midodrine is a prodrug converted in vivo to an active compound Apraclonidine and brimonidine used topically for glaucoma and ocular hypertension Methyldopa is converted in CNS to a-methyl NE, an effective a2 agonist

Schedule II drugs Marked tolerance occurs Chronic use leads to dependence Can result in hemorrhagic stroke in patients with underlying disease Long-term use can cause paranoid schizophrenia

(Continued)

Summary of Adrenergic Agonists and Antagonists (Continued)

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